Epidermal cell growth factors receptors (EGFR) are identified as one significant driving factor in the process for cellular growth and proliferation. The epidermal cell growth factors receptors family is composed of EGFR (Erb-B1), Erb-B2 (HER-2/neu), Erb-B3 and Erb-B4. The epidermal cell growth factor receptors are associated with the process for most cancers, such as lung cancer, colon cancer, breast cancer and the like. The overexpression and mutation of EGFR have been proved to be the leading risk factor for a breast cancer with poor prognosis.
The current edge-cutting research is focused on an irreversible third-generation EGFR inhibitor. The patent application CN201410365911.4 discloses the following compound of formula (I), which compound has a substantially higher inhibition activity to the EGFR activating mutation (such as exon 19 deletion activating mutation, or L858R activating mutation) and T790M resistance mutation than the inhibition activity to the wild-type EGFR (WT EGFR), with a good selectivity, a relatively low toxicity side-effect and a good safety.
